Vilazodone

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Vilazodone
Vilazodone.svg
Molecular structure of vilazodone
Vilazodone 3D.png
3D representation of a vilazodone molecule
Clinical data
Pronunciation /vɪˈlæzədoʊn/
vi-LAZ-ə-dohn
Trade names Viibryd
Other namesEMD-68843; SB-659746A
AHFS/Drugs.com Monograph
MedlinePlus a611020
License data
Routes of
administration 		By mouth
Drug class Serotonin modulator [1]
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability 72% (oral, with food) [5]
Metabolism Liver via CYP3A4 [5]
Elimination half-life 25 hours [5]
Excretion Faecal and renal [5]
Identifiers
  • 5-(4-[4-(5-Cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
Chemical and physical data
Formula C26H27N5O2
Molar mass 441.535 g·mol−1
3D model (JSmol)
  • N#Cc5ccc4[nH]cc(CCCCN3CCN(c2ccc1oc(C(N)=O)cc1c2)CC3)c4c5
  • InChI=1S/C26H27N5O2/c27-16-18-4-6-23-22(13-18)19(17-29-23)3-1-2-8-30-9-11-31(12-10-30)21-5-7-24-20(14-21)15-25(33-24)26(28)32/h4-7,13-15,17,29H,1-3,8-12H2,(H2,28,32) Yes check.svgY
  • Key:SGEGOXDYSFKCPT-UHFFFAOYSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Vilazodone, sold under the brand name Viibryd among others, is a medication used to treat major depressive disorder. [1] It is classified as a serotonin modulator [1] and is taken by mouth. [1]

Contents

Its common side effects include nausea, diarrhea, and trouble sleeping. [1] Serious side effects may include increased suicidal thoughts or actions in those under the age of 25, serotonin syndrome, bleeding, activation of mania or hypomania, pancreatitis, seizures, angle-closure glaucoma, sleep paralysis, and sexual dysfunction. [6]

Vilazodone may cause a syndrome of inappropriate antidiuretic hormone secretion (SIADH). [1] A withdrawal syndrome may occur if the dose is rapidly decreased. [1] Use during pregnancy and breastfeeding is not generally recommended. [7] It is in the serotonin modulator class of medications and is believed to work both as a selective serotonin reuptake inhibitor (SSRI) and activator of the 5-HT1A receptor. [1]

Vilazodone was approved for medical use in the United States in 2011 [1] and in Canada in 2018. [8] In 2019, it was the 334th most commonly prescribed medication in the United States, with more than 900 thousand prescriptions. [9] The drug lost patent protection in June 2022 for adults and in July 2023 for pediatrics. [10] Generic versions have been approved by the US Food and Drug Administration. [11] [12]

Medical uses

Seven controlled efficacy trials were conducted of vilazodone for treatment of major depressive disorder. [13] Five of these trials showed no significant influence of vilazodone over placebo on depressive symptoms. [13] In the remaining two trials, small but significant advantages of vilazodone over placebo were found. [13] [14] According to these two eight-week trials in adults, vilazodone has an antidepressant response after one week of treatment. [15] After eight weeks it resulted in a 13% greater response than placebo. [15] Remission rates, however, were not significantly different versus placebo. [15]

According to the US Food and Drug Administration (FDA) in 2011, "it is unknown whether vilazodone has any advantages compared to other drugs in the antidepressant class." [16] A 2019 review stated that "present studies do not suggest the superiority of vilazodone compared with other antidepressants." [17]

Development of vilazodone for generalized anxiety disorder has been stopped as of 2017. [18] While there is tentative evidence of a small benefit in generalized anxiety disorder, there is a high rate of side effects. [19]

Adverse effects

In September 2016, the US Food and Drug Administration (FDA) required a new warning to be added to the prescribing information related to a link between vilazodone and acute pancreatitis and sleep paralysis. [20] In addition, other sleep disturbances such as hypnagogic hallucinations and sleep terrors can occur. [21] [22]

Sleep paralysis is a state, during waking up or falling asleep, in which a person is conscious but experiences full-body paralysis. During an episode, the person may hallucinate (hear, feel, or see things that are not there), which often results in fear. [23] A night terror, also called sleep terror, is a sleep disorder causing feelings of panic or dread. [24] The rate of sleep paralysis adverse events was high enough to merit an FDA warning added to the Viibryd prescription label. [6] [21]

In July 2021, the US Food and Drug Administration required a new warning to be added to the prescription label that vilazodone may cause sexual dysfunction. Per the FDA label, sexual dysfunction can include ejaculatory delay or failure, decreased libido, and erectile dysfunction in male patients. In female patients, sexual dysfunction can include decreased libido and delayed or absent orgasm. [6]

The most common adverse effects include nausea, diarrhea, vomiting, and insomnia. [5]

After a one-year, open-label study assessing the safety and tolerability of vilazodone in people with major depressive disorder, the most common adverse effects were diarrhea (35.7%), nausea (31.6%), and headache (20.0%); greater than 90% of these adverse effects were mild or moderate. [25] [15] In randomized controlled trials, meanwhile, these rates were 28%, 23.4% and 13.3%, respectively. [15] In contrast to other selective serotonin reuptake inhibitors (SSRIs), initial trials showed that vilazodone did not cause decreased sexual desire/function, which often cause people to abandon their use. [26] [ unreliable medical source? ] However, post-marketing experience led the FDA to warn that vilazodone may cause sexual dysfunction. [6]

Pregnancy

Antidepressant exposure (including vilazodone) is associated with shorter average duration of pregnancy (by three days), increased risk of preterm delivery (by 55%), lower birth weight (by 75 g), and lower Apgar scores (by <0.4 points). [27] [28] It is uncertain whether there is an increased rate of septal heart defects among children whose mothers were prescribed an SSRI in early pregnancy. [29] [30]

Pharmacology

Pharmacodynamics

Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 2.1 nM; Ki = 0.1 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60–70%). [15] [31] It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C, [31] [32] as well as the norepinephrine and dopamine transporters (Ki = 56 nM for NET and 37 nM for DAT). [5] A small clinical study found occupancy of the 5-HT1A receptor with vilazodone, whereas occupancy of the SERT by vilazodone in humans does not seem to have been studied. [33] [34] [35] It has also been identified as a potent vesicular monoamine transporter 2 (VMAT2) inhibitor (IC50 Tooltip half-maximal inhibitory concentration = 69 nM). [36]

Pharmacokinetics

Vilazodone is best absorbed with food and has a bioavailability of 72% under fed conditions. The Cmax increased between 147 and 160% and the AUC increased between 64 and 85% of vilazodone when it was administered with either a fatty or light meal. [37]

History

It was developed by Merck KGaA and licensed by Clinical Data, a biotech company purchased by Forest Laboratories in 2011. [38]

References

  1. 1 2 3 4 5 6 7 8 9 "Vilazodone Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved March 3, 2019.
  2. ↑ Anvisa (March 31, 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published April 4, 2023). Archived from the original on August 3, 2023. Retrieved August 16, 2023.
  3. ↑ "Viibryd Product information". Health Canada. April 25, 2012. Retrieved June 10, 2022.
  4. ↑ "Health Canada New Drug Authorizations: 2015 Highlights". Health Canada . May 4, 2016. Retrieved April 7, 2024.
  5. 1 2 3 4 5 6 7 "Viibryd (vilazodone hydrochloride) tablet Viibryd (vilazodone hydrochloride) kit [Forest Laboratories, Inc.]". DailyMed. Forest Laboratories, Inc. December 2012. Archived from the original on October 29, 2013. Retrieved October 28, 2013.
  6. 1 2 3 4 "label" (PDF). Vilazodone label. U.S. Food and Drug Administration (FDA). July 1, 2021. Retrieved September 24, 2025.
  7. ↑ "Vilazodone (Viibryd) Use During Pregnancy". Drugs.com. Retrieved March 21, 2019.
  8. ↑ "Drug Product Database Online Query". Health Canada. Government of Canada. April 25, 2012. Retrieved May 18, 2020.
  9. ↑ "Vilazodone - Drug Usage Statistics". ClinCalc. Archived from the original on July 8, 2020. Retrieved October 16, 2021.
  10. ↑ "Generic Viibryd Availability".
  11. ↑ "Vilazodone: FDA-Approved Drugs". Archived from the original on May 1, 2017.
  12. ↑ "2019 First Generic Drugs Approvals". U.S. Food and Drug Administration (FDA). January 21, 2021. Archived from the original on August 5, 2020. Retrieved June 10, 2022.
  13. 1 2 3 Kirsch I (2014). "Antidepressants and the Placebo Effect". Zeitschrift für Psychologie. 222 (3): 128–134. doi:10.1027/2151-2604/a000176. PMC   4172306 . PMID   25279271.
  14. ↑ Wang SM, Han C, Lee SJ, Patkar AA, Masand PS, Pae CU (May 20, 2016). "Vilazodone for the Treatment of Depression: An Update". Chonnam Medical Journal. 52 (2): 91–100. doi:10.4068/cmj.2016.52.2.91.
  15. 1 2 3 4 5 6 Wang SM, Han C, Lee SJ, Patkar AA, Masand PS, Pae CU (August 2013). "A review of current evidence for vilazodone in major depressive disorder". International Journal of Psychiatry in Clinical Practice. 17 (3): 160–169. doi:10.3109/13651501.2013.794245. PMID   23578403. S2CID   10702028.
  16. ↑ Laughren TP, Gobburu J, Temple RJ, Unger EF, Bhattaram A, Dinh PV, et al. (September 2011). "Vilazodone: clinical basis for the US Food and Drug Administration's approval of a new antidepressant". The Journal of Clinical Psychiatry. 72 (9): 1166–1173. doi:10.4088/JCP.11r06984. PMID   21951984.
  17. ↑ Stuivenga M, Giltay EJ, Cools O, Roosens L, Neels H, Sabbe B (February 2019). "Evaluation of vilazodone for the treatment of depressive and anxiety disorders". Expert Opinion on Pharmacotherapy. 20 (3). Informa UK Limited: 251–260. doi:10.1080/14656566.2018.1549542. hdl: 1887/3630582 . PMID   30475091. S2CID   53773793.
  18. ↑ "New Medicines Newsletter" (PDF). NHS. Archived from the original (PDF) on March 21, 2019. Retrieved March 21, 2019.
  19. ↑ Zareifopoulos N, Dylja I (April 2017). "Efficacy and tolerability of vilazodone for the acute treatment of generalized anxiety disorder: A meta-analysis". Asian Journal of Psychiatry. 26: 115–122. doi:10.1016/j.ajp.2017.01.016. PMID   28483071.
  20. ↑ "SUPPLEMENT APPROVAL" (PDF). U.S. Food and Drug Administration (FDA). Archived from the original (PDF) on February 18, 2017.
  21. 1 2 Jiang Y, Qu Y, Du Z, Ou M, Shen Y, Zhou Q, et al. (May 2024). "Exploring adverse events of Vilazodone: evidence from the FAERS database". BMC Psychiatry. 24 (1): 371. doi: 10.1186/s12888-024-05813-0 . PMC   11100245 . PMID   38755677.
  22. ↑ Mancano MA (February 2018). "ISMP Adverse Drug Reactions: Influenza Vaccine-Induced Stevens-Johnson Syndrome; Vilazodone-Induced Nightmares; Dabigatran-Induced Pustular Eruptions; Neurotoxic and Cardiotoxic Symptoms After Cannabis Concentrate Exposure; Rosuvastatin-Induced Skin Eruption". Hospital Pharmacy. 53 (1): 15–17. doi:10.1177/0018578717739727. ISSN   0018-5787. PMC   5805017 . PMID   29434381.
  23. ↑ "Sleep paralysis". nhs.uk. October 23, 2017. Retrieved January 12, 2026.
  24. ↑ Sateia MJ (November 2014). "International Classification of Sleep Disorders-Third Edition". Chest. 146 (5): 1387–1394. doi:10.1378/chest.14-0970. ISSN   0012-3692.
  25. ↑ Robinson DS, Kajdasz DK, Gallipoli S, Whalen H, Wamil A, Reed CR (October 2011). "A 1-year, open-label study assessing the safety and tolerability of vilazodone in patients with major depressive disorder". Journal of Clinical Psychopharmacology. 31 (5): 643–6. doi:10.1097/JCP.0b013e31822c6741. PMID   21869687.
  26. ↑ "FDA approves Clinical Data Inc's antidepressant". Reuters. January 22, 2011. Archived from the original on January 27, 2011.
  27. ↑ Ross LE, Grigoriadis S, Mamisashvili L, Vonderporten EH, Roerecke M, Rehm J, et al. (April 2013). "Selected pregnancy and delivery outcomes after exposure to antidepressant medication: a systematic review and meta-analysis". JAMA Psychiatry. 70 (4): 436–443. doi: 10.1001/jamapsychiatry.2013.684 . PMID   23446732.
  28. ↑ Lattimore KA, Donn SM, Kaciroti N, Kemper AR, Neal CR, Vazquez DM (September 2005). "Selective serotonin reuptake inhibitor (SSRI) use during pregnancy and effects on the fetus and newborn: a meta-analysis". Journal of Perinatology. 25 (9): 595–604. doi: 10.1038/sj.jp.7211352 . PMID   16015372.
  29. ↑ Pedersen LH, Henriksen TB, Vestergaard M, Olsen J, Bech BH (September 2009). "Selective serotonin reuptake inhibitors in pregnancy and congenital malformations: population based cohort study". BMJ. 339 (sep23 1) b3569. doi:10.1136/bmj.b3569. PMC   2749925 . PMID   19776103.
  30. ↑ Huybrechts KF, Palmsten K, Avorn J, Cohen LS, Holmes LB, Franklin JM, et al. (June 2014). "Antidepressant use in pregnancy and the risk of cardiac defects". The New England Journal of Medicine. 370 (25): 2397–2407. doi:10.1056/NEJMoa1312828. PMC   4062924 . PMID   24941178.
  31. 1 2 Hughes ZA, Starr KR, Langmead CJ, Hill M, Bartoszyk GD, Hagan JJ, et al. (March 2005). "Neurochemical evaluation of the novel 5-HT1A receptor partial agonist/serotonin reuptake inhibitor, vilazodone". European Journal of Pharmacology. 510 (1–2): 49–57. doi:10.1016/j.ejphar.2005.01.018. PMID   15740724.
  32. ↑ Page ME, Cryan JF, Sullivan A, Dalvi A, Saucy B, Manning DR, et al. (September 2002). "Behavioral and neurochemical effects of 5-(4-[4-(5-Cyano-3-indolyl)-butyl)-butyl]-1-piperazinyl)-benzofuran-2-carboxamide (EMD 68843): a combined selective inhibitor of serotonin reuptake and 5-hydroxytryptamine(1A) receptor partial agonist". The Journal of Pharmacology and Experimental Therapeutics. 302 (3): 1220–1227. doi:10.1124/jpet.102.034280. PMID   12183683. S2CID   12020750.
  33. ↑ Dawson LA (December 2013). "The discovery and development of vilazodone for the treatment of depression: a novel antidepressant or simply another SSRI?". Expert Opinion on Drug Discovery. 8 (12): 1529–1539. doi:10.1517/17460441.2013.855195. PMID   24195711. S2CID   19662281.
  34. ↑ Dawson LA, Watson JM (2009). "Vilazodone: a 5-HT1A receptor agonist/serotonin transporter inhibitor for the treatment of affective disorders". CNS Neuroscience & Therapeutics. 15 (2): 107–117. doi:10.1111/j.1755-5949.2008.00067.x. PMC   6493994 . PMID   19499624.
  35. ↑ Choi E, Zmarlicka M, Ehret MJ (September 2012). "Vilazodone: a novel antidepressant". American Journal of Health-System Pharmacy. 69 (18): 1551–1557. doi:10.2146/ajhp110374. PMID   22935937.
  36. ↑ Racz R, Kozell LB, Eshleman AJ, Bloom SH, Wolfrum KM, Schmachtenberg JL, et al. (December 22, 2025). "Evaluation of the Relationship between Vesicular Monoamine Transporter 2 (VMAT2) Inhibition and Neurologic Adverse Events in Approved Drugs". ACS Pharmacology & Translational Science. doi:10.1021/acsptsci.5c00538. ISSN   2575-9108.
  37. ↑ Cruz MP (January 2012). "Vilazodone HCl (Viibryd): A Serotonin Partial Agonist and Reuptake Inhibitor For the Treatment of Major Depressive Disorder". P & T. 37 (1): 28–31. PMC   3278186 . PMID   22346333.
  38. ↑ "Xconomy: Blend Therapeutics Taps Former Clinical Data Chief Fromkin As New CEO". xconomy.com. April 13, 2015. Archived from the original on September 9, 2017. Retrieved May 6, 2018.
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